PI-145 (INK1197)是PI3K δ和γ高度选择性抑制剂,Ki和IC50分别为23 pM/243 pM和1 nM/50 nM。
Duvelisib (IPI-145, INK1197) is a novel and selective PI3K δ/γ inhibitor with Ki and IC50 of 23 pM/243 pM and 1 nM/50 nM in cell-free assays, highly selective for PI3K δ/γ than other protein kinases.
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Vito Palombella, Targeting PI3K- δ and PI3K-γ in Inflammation, 2012.
分子式 C22H17ClN6O |
分子量 416.86 |
CAS号 1201438-56-3 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 80 mg/mL |
Water <1 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT02598570 | Lymphoma | Drug: duvelisib | AbbVie|Infinity Pharmaceuticals, Inc. | Phase 1 | 2015-11-01 | 2017-02-03 |
NCT02095587 | Hepatic Impairment | Drug: IPI-145 | Verastem, Inc. | Phase 1 | 2014-03-01 | 2017-02-21 |
NCT02711852 | Hematologic Malignancy | Drug: Duvelisib | Verastem, Inc. | Phase 2 | 2016-04-01 | 2017-03-07 |
NCT02783625 | Lymphoma|Relapsed/Refractory T-cell Lymphomas | Drug: Romidepsin|Drug: Bortezomib|Drug: duvelisib | Memorial Sloan Kettering Cancer Center|Dana-Farber Cancer Institute|Stanford University | Phase 1 | 2016-05-01 | 2017-03-02 |
NCT02292225 | Lymphocytic Leukemia, Chronic|Lymphoma, Small Lymphocytic | Drug: IPI-145 (duvelisib)|Drug: Obinutuzumab | Verastem, Inc. | Phase 1 | 2015-02-01 | 2017-02-21 |
NCT01882803 | Indolent Non-Hodgkin Lymphoma | Drug: IPI-145 (duvelisib) | Verastem, Inc. | Phase 2 | 2013-05-01 | 2017-02-21 |
NCT02576275 | Indolent Non-Hodgkin's Lymphoma|Follicular Lymphoma|Small Lymphocytic Lymphoma|Marginal Zone Lymphoma | Drug: Duvelisib|Drug: Placebo|Drug: Rituximab|Drug: Bendamustine | Verastem, Inc. | Phase 3 | 2015-12-01 | 2017-02-21 |
NCT02307461 | Healthy | Drug: IPI-145 (duvelisib)|Drug: IPI-145|Drug: IPI-145 | Verastem, Inc. | Phase 1 | 2014-11-01 | 2017-02-21 |
NCT02640833 | Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma|Non-Hodgkin Lymphoma | Drug: Duvelisib|Drug: Venetoclax | AbbVie|Infinity Pharmaceuticals, Inc. | Phase 1 | 2016-07-01 | 2016-07-22 |
NCT02204982 | Follicular Lymphoma | Drug: IPI-145 (duvelisib)|Drug: Placebo|Drug: Rituximab | Verastem, Inc. | Phase 3 | 2014-09-01 | 2017-02-21 |
NCT02391545 | CD20+ Follicular Lymphoma | Drug: IPI-145 (duvelisib)|Drug: Rituximab|Drug: Obinutuzumab | Verastem, Inc. | Phase 1|Phase 2 | 2014-12-01 | 2017-03-23 |
NCT02004522 | Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma | Drug: IPI-145 (duvelisib)|Drug: Ofatumumab | Verastem, Inc. | Phase 3 | 2013-11-01 | 2017-03-23 |
NCT02049515 | Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma | Drug: IPI-145 (duvelisib)|Drug: Ofatumumab | Verastem, Inc. | Phase 3 | 2013-12-01 | 2017-02-21 |
NCT01653756 | Asthma | Drug: IPI-145, a PI3K Inhibitor|Drug: Placebo to match IPI-145 | Verastem, Inc. | Phase 2 | 2012-07-01 | 2017-02-21 |
NCT01476657 | Hematologic Malignancies | Drug: IPI-145 (duvelisib) | Verastem, Inc. | Phase 1 | 2011-10-01 | 2017-02-21 |
NCT01836861 | Healthy | Drug: IPI-145 | Verastem, Inc. | Phase 1 | 2013-03-01 | 2017-02-21 |
NCT01549106 | Healthy Volunteers | Drug: IPI-145|Drug: Placebo | Verastem, Inc. | Phase 1 | 2011-08-01 | 2017-02-21 |
NCT01851707 | Rheumatoid Arthritis | Drug: IPI-145|Drug: Placebo | Verastem, Inc. | Phase 2 | 2013-04-01 | 2017-02-21 |
NCT01871675 | Lymphoma|Chronic Lymphocytic Leukemia|Non-Hodgkin Lymphoma|T-cell Lymphoma | Drug: IPI-145|Drug: Rituximab|Drug: Bendamustine | SCRI Development Innovations, LLC|Infinity Pharmaceuticals, Inc. | Phase 1 | 2013-05-01 | 2016-07-07 |
NCT02605694 | Lymphoma | Drug: Duvelisib|Drug: Rituximab|Drug: R-CHOP|Drug: Prednisone | Verastem, Inc. | Phase 2 | 2015-12-01 | 2017-02-21 |
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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